ACARBOSE

What it is

Glybosay is an alpha-glucosidase inhibitor that works by inhibiting intestinal enzymes involved in the degradation of ingested disaccharides, oligosaccharides, and polysaccharides. This leads to delayed digestion of carbohydrates, so that absorbable monosaccharides originating from carbohydrates are released more slowly and taken up into blood more slowly. In this way, Glybosay reduces the postprandial rise in blood glucose, truncates blood-glucose fluctuations throughout the day, and reduces the mean blood-glucose level.

Approved indications

— Adjunct to prescribed diet and exercise for the management of blood glucose concentrations in non-insulin dependent diabetic patients who are inadequately controlled by diet alone or by diet and oral hypoglycaemic agents.

Dosing overview

The optimal dosage of Glybosay must be individualised, as the activity and tolerability varies from individual to individual. In adults, Glybosay should be started at a low initial dose and increased slowly to minimise gastrointestinal side effects, usually commencing at 50 mg once daily for the first week, 50 mg twice daily for the second week, and 50 mg three times a day for the third week. A further increase of the dose may be necessary after 4–8 weeks on the basis of blood glucose level, with the average adult dose being 100 mg three times daily. A further increase to 200 mg three times daily may occasionally be necessary. Glybosay should be swallowed whole with a little liquid directly before a meal or chewed with the first few mouthfuls of the meal.

Key safety warnings

Ingestion of sucrose and food containing sucrose can easily lead to considerable intestinal symptoms such as flatulence and bloating, or even diarrhoea during treatment with Glybosay, as a result of increased carbohydrate fermentation in the colon. Whilst Glybosay has an antihyperglycaemic effect, it does not itself induce hypoglycaemia; however, if Glybosay is prescribed in addition to drugs containing sulfonylureas or metformin or in addition to insulin, a fall of blood glucose levels into the hypoglycaemic range may necessitate a suitable decrease in the sulfonylurea, metformin or insulin dose. In the event of acute hypoglycaemia, cane sugar (sucrose) is broken down into fructose and glucose more slowly during Glybosay treatment and is therefore unsuitable for rapid elimination of hypoglycaemic phenomena; glucose (dextrose) should be used in place of cane sugar. Patients' liver enzyme values should be monitored regularly, preferably at monthly intervals for the first 6 to 12 months after initiation of Glybosay therapy, and if elevated transaminases are observed, a reduction in dosage or withdrawal of therapy may be warranted, particularly if the elevations persist. Cases of fulminant hepatitis have been reported during Glybosay therapy.

Contraindications

Glybosay is contraindicated in patients with hypersensitivity to acarbose and/or any of the inactive tablet constituents, pregnancy, and lactation. Glybosay should not be used in patients under 18 years of age. Glybosay is contraindicated in patients with severe renal impairment (creatinine clearance <25 mL/min). Glybosay is contraindicated in patients with severe hepatic impairment. Glybosay should not be used in patients with gastrointestinal disorders associated with malabsorption, inflammatory bowel disease (such as ulcerative colitis and Crohn's disease), colonic ulceration, partial intestinal obstruction, or in patients predisposed to intestinal obstruction or ileus. Glybosay should not be used in patients with chronic intestinal diseases associated with marked disorders of digestion or absorption and in patients who suffer from states which may deteriorate as a result of increased gas formation in the intestine (such as Roemheld syndrome, major hernias, intestinal obstruction and intestinal ulcers). Glybosay is contraindicated in patients with diabetic ketoacidosis.

Regulatory history

Glybosay was first approved on 14 May 2015.